This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. High throughput screening (HTS) has become a powerful tool for biomedical research and a resource for drug discovery. The purpose of HTS is to screen large numbers of small molecules that interact selectively with biological targets so that they may be used as probes to understand the function of newly characterized proteins and to analyze physiological e processes, cellular phenomena, and disease mechanisms. The HTS laboratory at the University of Kansas (www.hts.ku.edu) was established through the COBRE grant and has provided service to COBRE investigators, and the local and national research community. We have supported and will continue to support COBRE investigators and will also expand both the scope and capacity of our high throughput screening to meet the increased needs of biomedical researchers. Our objectives are (1) to strengthen our assay development capacity to import and adapt biochemical and cell-based assays to HTS format and (2) to strengthen our high throughput screening capacity to carry out efficient screening campaigns. We work with individual research investigators to adapt their bench-top assays to suit HTS operation and use these successfully adapted HTS assays to screen our existing chemical library of small organic compounds for molecules showing biological activity. Because of the existing HTS facility and personnel at the University of Kansas, we are certain that further expansion will make significant contributions toward the discovery of new interesting compounds and toward the design, synthesis and evaluation of analogues derived from original hits coming from HTS.